Abstract
A new class of 4-thiazolidinones clubbed with quinozolinone nucleus has been synthesized. The title compounds were screened for their in vitro antimicrobial and anticancer potentials. Results of antimicrobial and anticancer study revealed that compounds 7 (pMICam = 1.69 μM/ml) and 2 (IC50 = 12.83 μM) were found to be the most potent antimicrobial and anticancer agents respectively. QSAR studies indicated that antimicrobial activity of synthesized 4-thiazolidinone derivatives was governed by the electronic parameters, dipole moment (μ), energy of highest occupied molecular orbital (HOMO), lipophilic parameter, log P and topological parameter, valence third order molecular connectivity index (3χv).
Keywords: 4-Thiazolidinones, Antibacterial, Anticancer, Antifungal, QSAR, Synthesis.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Synthesis, Antimicrobial, Anticancer Evaluation of 2-(aryl)-4- Thiazolidinone Derivatives and their QSAR Studies
Volume: 15 Issue: 11
Author(s): Aakash Deep, Pradeep Kumar, Balasubramanian Narasimhan, Kalavathy Ramasamy, Vasudevan Mani, Rakesh Kumar Mishra and Abu Bakar Abdul Majeed
Affiliation:
Keywords: 4-Thiazolidinones, Antibacterial, Anticancer, Antifungal, QSAR, Synthesis.
Abstract: A new class of 4-thiazolidinones clubbed with quinozolinone nucleus has been synthesized. The title compounds were screened for their in vitro antimicrobial and anticancer potentials. Results of antimicrobial and anticancer study revealed that compounds 7 (pMICam = 1.69 μM/ml) and 2 (IC50 = 12.83 μM) were found to be the most potent antimicrobial and anticancer agents respectively. QSAR studies indicated that antimicrobial activity of synthesized 4-thiazolidinone derivatives was governed by the electronic parameters, dipole moment (μ), energy of highest occupied molecular orbital (HOMO), lipophilic parameter, log P and topological parameter, valence third order molecular connectivity index (3χv).
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Cite this article as:
Deep Aakash, Kumar Pradeep, Narasimhan Balasubramanian, Ramasamy Kalavathy, Mani Vasudevan, Kumar Mishra Rakesh and Abdul Majeed Abu Bakar, Synthesis, Antimicrobial, Anticancer Evaluation of 2-(aryl)-4- Thiazolidinone Derivatives and their QSAR Studies, Current Topics in Medicinal Chemistry 2015; 15 (11) . https://dx.doi.org/10.2174/1568026615666150317221849
DOI https://dx.doi.org/10.2174/1568026615666150317221849 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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